# US 9,000,023 B2 · Disubstituted phthalazine hedgehog pathway antagonists

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- Number: US 9,000,023 B2
- Document ID: US9000023B2
- Status: Granted
- Kind: B2
- Application number: 13/590,481
- Filed: 2012-08-21
- Published: 2012-12-13
- Granted: 2015-04-07
- Earliest claimed: 2009-06-19
- Assignees: Eli Lilly and Company
- Applicants: Philip Arthur Hipskind; Bharvin Kumar Patel; Takako Wilson (nee Takakuwa)
- Inventors: Philip Arthur Hipskind; Bharvin Kumar Patel; Takako Wilson (nee Takakuwa)
- Web page: https://patentgrep.com/patent/US9000023B2

## CPC

- C07D 401/14: containing three or more hetero rings
- A61P 25/02: for peripheral neuropathies
- A61P 35/00: Antineoplastic agents
- A61P 35/02: specific for leukemia
- A61P 35/04: specific for metastasis
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention provides novel 1,4-disubstituted phthalazine hedgehog pathway antagonists useful in the treatment of cancer.

## Claims

### Claim 1

A method of treating cancer selected from the group consisting of brain cancer, basal cell carcinoma, esophagus cancer, gastric cancer, pancreatic cancer, biliary tract cancer, prostate cancer, breast cancer, small-cell lung cancer, non-small cell lung cancer, B-cell lymphoma, multiple myeloma, ovarian cancer, colorectal cancer, liver cancer, kidney cancer, melanoma, head and neck cancer, soft tissue sarcomas, bone sarcomas, and leukemia in a mammal comprising administering to the mammal an effective amount of a compound which is 4-fluoro-N-methyl-N-(1-(4-(1-methyl-1H-pyrazol-5-yl)phthalazin-1-yl)piperidin-4-yl)-2-(trifluoromethyl)benzamide, or a pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

The method according to claim 1 wherein the cancer is basal cell carcinoma.

### Claim 3 (depends on 1)

The method according to claim 1 wherein the cancer is pancreatic cancer.

### Claim 4 (depends on 1)

The method according to claim 1 wherein the cancer is brain cancer.

### Claim 5 (depends on 4)

The method according to claim 4 wherein the brain cancer is medulloblastoma.

### Claim 6 (depends on 1)

The method according to claim 1 wherein the cancer is small-cell lung cancer.